Absorption, Distribution and Excretion
After oral administration, it is well absorbed via the gastrointestinal tract. Metabolisms/Metabolites In dogs and humans, the major urinary metabolite of benzoyldiphenyl ether is N-(4,4-diphenyl-4-hydroxybutyl)-δ-aminovaleric acid (not less than 50% of the dose). Secondary urinary metabolites include a phenolic compound and a lactam compound. Biological Half-Life 4 hours

Non-Human Toxicity Values
Mice oral LD50: 430 mg/kg/hydrochloride/
Mice intraperitoneal LD50: 105 mg/kg/hydrochloride/
Mice intravenous LD50: 37 mg/kg/hydrochloride/
Rat oral LD50: 515 mg/kg/hydrochloride/
For more complete non-human toxicity data for dibenzoneols (6 in total), please visit the HSDB record page.

Neurosci Lett.2015 Mar 4;589:62-6.

Difenidol is a tertiary alcohol, formed by replacing two phenyl groups at the 1-position of butan-1-ol and one piperidin-1-yl group at the 4-position. It is an antiemetic. It belongs to the piperidine class, tertiary alcohol class, and benzene class. Difenidol is an antiemetic used to treat vomiting and dizziness. Overdose of difenidol in children may lead to serious poisoning. Difenidol is an antiemetic. The physiological action of difenidol is through the suppression of vomiting. Drug Indications Used for the prevention and treatment of peripheral (labyrinthine) vertigo, as well as nausea and vomiting caused by Meniere's disease and middle or inner ear surgery. It can also be used to control nausea and vomiting caused by surgery, malignant tumors, labyrinthine dysfunction, antitumor drug therapy, radiation sickness, and infectious diseases. FDA Label Mechanism of Action The mechanism by which difenidol exerts its antiemetic and antivertigo effects is not fully understood. It is believed to reduce vestibular stimulation, inhibit labyrinthine function, and have anticholinergic effects. Its effect on the medullary chemoreceptor trigger zone may also contribute to its antiemetic effect. Diphenidol has no significant sedative, tranquilizing, or antihistamine effects. It has a weak peripheral anticholinergic effect.
Experiments have shown that it has a weak parasympathetic blocking effect, but lacks significant sedative, tranquilizing, or antihistamine properties.
.../Diphenidol/is believed to act on the vestibular organs of the ear...

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Therapeutic Uses
Anemetic; Histamine H1 receptor antagonist
...An antiemetic that can be taken orally, rectally, intramuscularly, or intravenously, used to treat nausea and vomiting caused by infectious diseases, malignant tumors, radiation sickness, general anesthesia, and antitumor drug treatment. ...It can also be used to treat vestibular vertigo.
In adults, this drug is also effective for...labyrinthitis after middle and inner ear surgery and Meniere's disease. Its efficacy in treating vertigo in children has not been studied. /HCL/

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Drug Warnings
Because difenidol has a parasympathetic blocking effect, it should be used with caution in patients with glaucoma, benign prostatic hyperplasia, peptic ulcers, pyloric or duodenal obstruction, or cardiac spasm.
...It is not recommended for use during pregnancy-related nausea and vomiting, as its safety in this condition has not been established.

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Pharmacodynamics
Difenidol is used to control nausea and vomiting. It has an anti-vertigo effect on the vestibular system, controlling nausea and vomiting by inhibiting chemoreceptor trigger zones, thereby preventing motion sickness.

C21H28CLNO

345.91

309.209

3254-89-5

26363-46-2 (pamoate);3254-89-5 (HCl);972-02-1;

3055

White to off-white solid powder

473.3ºC at 760 mmHg

212-214
104-105 °C

233.5ºC

4.126

1

2

6

23

307

0

AVZIYZHXZAYGJS-UHFFFAOYSA-N

InChI=1S/C21H27NO.ClH/c23-21(19-11-4-1-5-12-19,20-13-6-2-7-14-20)15-10-18-22-16-8-3-9-17-22;/h1-2,4-7,11-14,23H,3,8-10,15-18H2;1H

1,1-Diphenyl-4-piperidin-1-ylbutan-1-ol hydrochloride

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility in Formulation 1: ≥ 2.5 mg/mL (7.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (7.23 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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 (Please use freshly prepared in vivo formulations for optimal results.)